II. Indications

III. Contraindications

IV. Mechanism

  1. Anti-Folate agent active as an antineoplastic and Immunosuppressant
  2. Targets cells expressing RFC-1 (reduced Folate carrier-1)
  3. Folate analog inhibitor of dihydrofolate reductase (DHFR)
    1. Blocks Tetrahydrofolate synthesis
    2. Depletes Nucleotide precursors
    3. Inhibits DNA, RNA and Protein synthesis

V. Medications

  1. Pralatrexate IV Solution 20 mg/ml in 1 to 2 ml vials

VI. Dosing

  1. See other references for disease specific dosing protocols
  2. Adult: 30 mg/m2 IV once weekly for 6 weeks, followed by 1 week of no Pralatrexate
  3. Coadministered agents to reduce adverse effects (e.g. mucositis)
    1. Folic Acid 1 to 1.25 mcg orally daily
      1. Start 10 days before, and continue for 30 days after last Pralatrexate dose
    2. Vitamin B12 1000 mcg IM
      1. Give one dose within 10 weeks of starting Pralatrexate
      2. Repeat Vitamin B12 dosing every 10 weeks while taking Pralatrexate

VII. Adverse Effects

  1. Hepatotoxicity
  2. Myelosuppression
  3. Mucositis
  4. Life-Threatening Drug-Induced Rashes (e.g. Toxic Epidermal Necrolysis)

VIII. Safety

  1. Avoid in Pregnancy (any trimester)
    1. Use reliable Contraception
  2. Avoid in Lactation

IX. Drug Interactions

  1. Drugs that prolong Pralatrexate activity (decreased clearance)
    1. NSAIDs
    2. Trimethoprim Sulfamethoxazole

Images: Related links to external sites (from Bing)

Related Studies